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Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2

[Image: see text] Leucine-rich repeat kinase 2 (LRRK2) is one of the most promising targets for Parkinson’s disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors, which, however, have limitations as the inhibited protein can interfere with natural mechanisms, which c...

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Detalles Bibliográficos
Autores principales: Liu, Xingui, Kalogeropulou, Alexia F., Domingos, Sofia, Makukhin, Nikolai, Nirujogi, Raja S., Singh, Francois, Shpiro, Natalia, Saalfrank, Anton, Sammler, Esther, Ganley, Ian G., Moreira, Rui, Alessi, Dario R., Ciulli, Alessio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9501899/
https://www.ncbi.nlm.nih.gov/pubmed/36007011
http://dx.doi.org/10.1021/jacs.2c05499